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Enprofylline

Cat. No. M30061
Enprofylline Structure
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Quality Control & Documentation
Biological Activity

Enprofylline acts as a selective and competitive A2B receptor antagonist with the Ki of 7 μM. Enprofylline also acts as a phosphodiesterase inhibitor. Enprofylline can be used for the research of asthma, chronic obstructive pulmonary disease.

Chemical Information
Molecular Weight 194.19
Formula C8H10N4O2
CAS Number 41078-02-8
Form Solid
Solubility (25°C) DMSO 62.5 mg/mL (ultrasonic)
Storage 4°C, protect from light
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] K R Chapman, et al. Chest. Long-term xanthine therapy of asthma. Enprofylline and theophylline compared. International Enprofylline Study Group

[2] M Esquivel, et al. Clin Pharmacol Ther. Cardiovascular effects of enprofylline and theophylline

[3] B J Chapman, et al. Br J Dis Chest. Enprofylline in chronic asthma

[4] C G Persson, et al. Life Sci. Effects of enprofylline and theophylline may show the role of adenosine

[5] I Muraoka, et al. Drug Metab Dispos. Pharmacokinetics and renal handling of enprofylline in pregnant rats

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Keywords: Enprofylline supplier, Adenosine Receptor, inhibitors, activators


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